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Biochem 2 > 14. Adrenergic receptors (adrenoceptors) - DOPAMIN > Flashcards

14. Adrenergic receptors (adrenoceptors) - DOPAMIN Flashcards

1
Q

Characteristics of adrenoceptors: α1 receptor
-> What is the main effect?

A

Constriction/Contraction

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2
Q

Characteristics of adrenoceptors: α1 receptor
-> Main effect: Constriction/Contraction

A

Blood vessels, bronchi, uterus, sphincters (GI, bladder),
iris (radial muscle)→midriasis
Liver hepatocytes: glycogenolysis

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3
Q

Examples of clinical use of adrenoceptors: α1 receptor

A

agonist:
hypotension
nasal congestion
used as a vasoconstrictor in local anesthetics to decrease their absorption

antagonist: hypertension; benign prostatic hypertrophy

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4
Q

Characteristics of adrenoceptors: α2 receptor
-> Main effects

A

presynaptic: feedback: inhibits NE release inhibits sympathetic (adrenergic) outflow

postsynaptic: vasoconstriction
pancreatic beta cells: decrease insulin secretion platelets: aggregation

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5
Q

Characteristics of adrenoceptors: α2 receptor
-> Example of clinical use (agonist)

A

hypertension treatment
(opiate) withdrawal treatment
vasomotor instability (‘hot flushes’)

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6
Q

Characteristics of adrenoceptors: α2 receptor
-> Example of clinical use (antagonist)

A

(not used clinically claimed to be aphrodisiac)

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7
Q

Glucose regulation of insulin secretion by ___- (which type of cells)

A

Pancreatic beta cell

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8
Q

Glucose regulation of insulin secretion by pancreatic beta cells

A

1/ Glucose transporter GLUT2
2/ ATP-gated K+ channel
3/ Voltage-gated Ca2+ channel

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9
Q

Where are Incretins (Glucagon-like peptide 1 [GLP-1]) released?

A

They are released from neuroendocrine cells of the gastrointestinal tract

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10
Q

Incretins (Glucagon-like peptide 1 [GLP-1])
are released from neuroendocrine cells of the gastrointestinal tract following food ingestion and amplify ___ and ___

A

glucose-stimulated insulin secretion and suppress glucagon secretion.

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11
Q

What are GLP-1 agonists?

A

pharmacologic agents that prolong the activity of endogenous GLP-1 enhance insulin secretion.

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12
Q

What does this slide indicate?

A

Structure of the β-adrenergic receptor in the active states and its associated trimeric G protein

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13
Q

What does this slide indicate?

A

Structure of the β-adrenergic receptor in the active states and its associated trimeric G protein

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14
Q

Characteristics of adrenoceptors: β1 receptor
-> What are the main effects of adrenoceptors: β1 receptor?

A

increase heart rate, force of contraction renin release
lipolysis

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15
Q

Characteristics of adrenoceptors: β1 receptor
-> What are the examples of clinical use (agonist)?

A

severe cardiac failure

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16
Q

Characteristics of adrenoceptors: β1 receptor
-> What are the examples of clinical use (antagonist)?

A

antagonist (beta blockers):
prevent heart ischemia

hypertension social fobia

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17
Q

Characteristics of adrenoceptors: β1 receptor
-> Identify 1

A

ACE inhibitors

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18
Q

Characteristics of adrenoceptors: β1 receptor
-> What can inhibit AT1 receptors?

A

Angiotensin II
AT1 subtype receptor antagonists

19
Q

Characteristics of adrenoceptors: β2 receptor
-> What is the main effect?

A

Main effect: dilate/relax

blood vessels, bronchi, uterus, GI, sphincter (bladder), ciliary muscle→miosis

Liver, muscle: glycogenolysis

Mast cells: inhibition of histamine release

20
Q

Characteristics of adrenoceptors: β2 receptor
-> What is an example of clinical use - agonist?

A

bronchodilators (asthma)
(also inhibit mediator release from mast cells)

21
Q

Characteristics of adrenoceptors: β2 receptor
-> Identify

A

cAMP-dependent protein kinase

22
Q

Characteristics of adrenoceptors: β2 receptor
-> What is happening at 1 & 2?

A

1/ Myosin light chain kinase is active
2/ Myosin light chain is phosphorylated

23
Q

Characteristics of adrenoceptors: β2 receptor
-> What is happening here?

A

reduced sensitivity of MLCK to the Ca2+ -calmodulin complex

24
Q

Characteristics of adrenoceptors: β2 receptor
-> What will happen at 1 & 2?

A

1/ contraction
2/ smooth muscle relaxation

25
Q

Characteristics of adrenoceptors: β3 receptor
-> What is the main effect?

A

relax bladder
lipolysis
thermogenesis

26
Q

Examples of clinical use of adrenoceptors: β3 receptor

A

agonist:
overactive bladder

27
Q

Identify

A
28
Q

Characteristics of VMAT 2 - vesicular monoamine transporter 2?

A

Broad substrate-specificity to biogenic amines
(tryptamine, tyramine, amphetamine – compete with endogenous catecholamine)

29
Q

Identify 1 & 2

A

1/ Dihydroxyphenylacetic acid (DOPAC)
2/ Homovanilic acid (HVA)

30
Q

List Dopaminergic receptors types

A
31
Q

Dopaminergic receptors
-> The role of D1 type

A
32
Q

Dopaminergic receptors
-> The role of D2 type

A
33
Q

Examples of endogenous Neurotoxins

A

metabolites of catabolism:
DOPAL

34
Q

Exogenous neurotoxins
-> The mechanism of MPTP

(1-methyl-4-phenyl- 1,2,3,6-tetrahydropyridine)

A

Taken up by dopaminergic nerve terminals – metabolized by MAO-B
-> 1-methyl-4-phenyl-pyridinium (MPP+) - active toxic metabolite – complex I inhibitor

35
Q

Exogenous neurotoxins
-> Where do MPTP present?

A

In the i.v. narcotic drug heroin as a contaminant

36
Q

The role of Cycad tree

A

tropical seed contains ß-methyl-amino- L-alanin (BMAA) produced by cyanobacteria found in the roots of cycads

37
Q

does Dopamine cross the blood-brain barrier?

A

Dopamine does not cross the blood-brain barrier (BBB)

38
Q

does Dopamine cross the blood-brain barrier?

A

Dopamine does not cross the blood-brain barrier (BBB)

39
Q

Drugs in therapy of Parkinson’s disease
-> name of these inhibitors

A
40
Q

Drugs in therapy of Parkinson’s disease
-> name of these inhibitors

A
41
Q

Drugs in therapy of Parkinson’s disease
-> Identify

A

Dopamine agonists act directly on dopamine receptors

42
Q

Dopaminergic reward system
-> What are the rewards?

A

Rewards: mediate the effects of reinforcement

43
Q

Dopaminergic reward system
-> What are the primary rewards?

A

necessary for survival (food, water, sexual contact, physical contact (cuddling), successful agression)

44
Q

Drugs interfere with Dopaminergic reward system
-> How?

A

Produce some of the effects of natural rewards (but not others, such as emotional effects, memory etc)

Biochem 2 (38 decks)

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